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1. 发明专利

IL261055A Tetrahydroisoquinoline derivatives 未知
公开(公告)号：IL261055A
公开(公告)日：2021-03-25
申请号：IL26105518
申请日：2018-08-08
申请人： ASTELLAS PHARMA INC , CYTOKINETICS INC , IPPEI SATO , TAKASHI KAMIKUBO , MASANORI MIURA , YUJI MATSUSHIMA , HIROAKI TANAKA , YASUHIRO SHIINA , SUSUMU YAMAKI , TOMOYUKI SAITO , HIROSHI KIYOHARA , MUNEMICHI OHE , KAYOKO MIHARA , BRADLEY PAUL MORGAN , FADY MALIK , SCOTT EMILE COLLIBEE , LUKE ASHCRAFT , PU PING LU , JEFFREY MICHAEL WARRINGTON , MARC GARARD
发明人： IPPEI SATO , TAKASHI KAMIKUBO , MASANORI MIURA , YUJI MATSUSHIMA , HIROAKI TANAKA , YASUHIRO SHIINA , SUSUMU YAMAKI , TOMOYUKI SAITO , HIROSHI KIYOHARA , MUNEMICHI OHE , KAYOKO MIHARA , BRADLEY PAUL MORGAN , FADY MALIK , SCOTT EMILE COLLIBEE , LUKE ASHCRAFT , PU-PING LU , JEFFREY MICHAEL WARRINGTON , MARC GARARD
IPC分类号： A61K31/47 , A61P21/00
摘要： Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.

2. 发明专利

IL261055D0 Tetrahydroisoquinoline derivatives 未知
公开(公告)号：IL261055D0
公开(公告)日：2018-10-31
申请号：IL26105518
申请日：2018-08-08
申请人： ASTELLAS PHARMA INC , CYTOKINETICS INC , IPPEI SATO , TAKASHI KAMIKUBO , MASANORI MIURA , YUJI MATSUSHIMA , HIROAKI TANAKA , YASUHIRO SHIINA , SUSUMU YAMAKI , TOMOYUKI SAITO , HIROSHI KIYOHARA , MUNEMICHI OHE , KAYOKO MIHARA , BRADLEY PAUL MORGAN , FADY MALIK , SCOTT EMILE COLLIBEE , LUKE ASHCRAFT , PU PING LU , JEFFREY MICHAEL WARRINGTON , MARC GARARD
发明人： IPPEI SATO , TAKASHI KAMIKUBO , MASANORI MIURA , YUJI MATSUSHIMA , HIROAKI TANAKA , YASUHIRO SHIINA , SUSUMU YAMAKI , TOMOYUKI SAITO , HIROSHI KIYOHARA , MUNEMICHI OHE , KAYOKO MIHARA , BRADLEY PAUL MORGAN , FADY MALIK , SCOTT EMILE COLLIBEE , LUKE ASHCRAFT , PU-PING LU , JEFFREY MICHAEL WARRINGTON , MARC GARARD
IPC分类号： C07D20060101
摘要： Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.

3. 发明申请

US20100105658A1 AZA-BRIDGED-RING COMPOUND 有权
标题翻译： AZA-BRIDGED-RING化合物
公开(公告)号：US20100105658A1
公开(公告)日：2010-04-29
申请号：US12524758
申请日：2008-02-07
申请人： Shinya Nagashima , Toru Kontani , Hiroshi Nagata , Yuji Matsushima , Hisao Hamaguchi , Tadatsura Koshika
发明人： Shinya Nagashima , Toru Kontani , Hiroshi Nagata , Yuji Matsushima , Hisao Hamaguchi , Tadatsura Koshika
IPC分类号： A61K31/439 , C07D453/02 , C07D223/14 , A61K31/55 , A61P29/00
CPC分类号： C07D453/02 , C07D471/18
摘要： [Problems] Provided is a compound which has an antagonistic action on a muscarinic M3 receptor and is useful as an active ingredient of a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.[Means for Solving Problems] The present inventors have made studies on a compound having an antagonistic action on the binding of a muscarinic M3 receptor, and they have found that an aza-bridged-ring compound or a salt thereof has an antagonistic action on the binding of a muscarinic M3 receptor, thereby completing the present invention. The aza-bridged-ring compound of the present invention has an antagonistic action on the binding of a muscarinic M3 receptor, and can be used as a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.
摘要翻译： [问题]提供对毒蕈碱M3受体具有拮抗作用的化合物，并且可用作炎性疾病如慢性阻塞性肺病（COPD），哮喘的预防和/或治疗剂的活性成分喜欢。解决问题的手段本发明人研究了对毒蕈碱性M3受体的结合具有拮抗作用的化合物，并且已经发现，氮杂桥环化合物或其盐对其有拮抗作用结合毒蕈碱M3受体，从而完成本发明。本发明的氮杂桥环化合物对毒蕈碱性M3受体的结合具有拮抗作用，可用作炎性疾病如慢性阻塞性肺疾病（COPD）的预防和/或治疗剂，，哮喘等。

4. 发明申请

US20050113387A1 Pyrazine derivatives and pharmaceutical use thereof 失效
标题翻译：吡嗪衍生物及其药物用途
公开(公告)号：US20050113387A1
公开(公告)日：2005-05-26
申请号：US10972340
申请日：2004-10-26
申请人： Satoshi Yonishi , Satoshi Aoki , Yuji Matsushima , Atsushi Akahane
发明人： Satoshi Yonishi , Satoshi Aoki , Yuji Matsushima , Atsushi Akahane
IPC分类号： A61K31/4965 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , A61K31/497 , C07D43/02 , C07D43/14
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14
摘要： A pyrazine derivative of the following formula (I): or a salt thereof. The pyrazine compound (I) and a salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.
摘要翻译：下式（I）的吡嗪衍生物或其盐。本发明的吡嗪化合物（I）及其盐是腺苷拮抗剂，可用于预防和/或治疗抑郁症，痴呆（例如阿尔茨海默氏病，脑血管性痴呆，伴有帕金森病的痴呆等），帕金森病，焦虑，疼痛，脑血管疾病（例如中风等），心力衰竭等。

5. 发明授权

US08367696B2 Aza-bridged-ring compound 有权
标题翻译：氮杂桥环化合物
公开(公告)号：US08367696B2
公开(公告)日：2013-02-05
申请号：US12524758
申请日：2008-02-08
申请人： Shinya Nagashima , Toru Kontani , Hiroshi Nagata , Yuji Matsushima , Hisao Hamaguchi , Tadatsura Koshika
发明人： Shinya Nagashima , Toru Kontani , Hiroshi Nagata , Yuji Matsushima , Hisao Hamaguchi , Tadatsura Koshika
IPC分类号： A61K31/439 , C07D221/00 , C07D221/02
CPC分类号： C07D453/02 , C07D471/18
摘要： [PROBLEMS] Provided is a compound which has an antagonistic action on a muscarinic M3 receptor and is useful as an active ingredient of a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.[MEANS For SOLVING PROBLEMS] The present inventors have made studies on a compound having an antagonistic action on the binding of a muscarinic M3 receptor, and they have found that an aza-bridged-ring compound or a salt thereof has an antagonistic action on the binding of a muscarinic M3 receptor, thereby completing the present invention. The aza-bridged-ring compound of the present invention has an antagonistic action on the binding of a muscarinic M3 receptor, and can be used as a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.
摘要翻译： [问题]提供对毒蕈碱M3受体具有拮抗作用并可用作炎性疾病如慢性阻塞性肺疾病（COPD），哮喘的预防和/或治疗剂的活性成分的化合物喜欢。解决问题的手段本发明人研究了对毒蕈碱性M3受体的结合具有拮抗作用的化合物，并且已经发现氮杂桥环化合物或其盐对其具有拮抗作用结合毒蕈碱M3受体，从而完成本发明。本发明的氮杂桥环化合物对毒蕈碱性M3受体的结合具有拮抗作用，可用作炎性疾病如慢性阻塞性肺疾病（COPD）的预防和/或治疗剂，，哮喘等。

6. 发明授权

US08524727B2 Pyrimidine compound 有权
标题翻译：嘧啶化合物
公开(公告)号：US08524727B2
公开(公告)日：2013-09-03
申请号：US12933137
申请日：2010-03-29
申请人： Yuji Matsushima , Hirokazu Kubota , Hisao Hamaguchi , Yoshinori Okamoto , Takeshi Hondo , Fusako Nishigaki
发明人： Yuji Matsushima , Hirokazu Kubota , Hisao Hamaguchi , Yoshinori Okamoto , Takeshi Hondo , Fusako Nishigaki
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07D239/42 , C07D239/34 , C07D239/38 , C07D239/48 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/06 , C07D451/04 , C07D453/02 , C07D491/107 , C07D493/08
摘要： A novel and excellent method for preventing and/or treating diseases related to a cannabinoid type 2 receptor, based on an agonistic action on a cannabinoid type 2 receptor. It was found that a hetero ring derivative mainly having two substituents, for example, a pyrimidine-5-carboxamide derivative having a substituent amino group at the 2-position, exhibits a potent agonistic action on a cannabinoid type 2 receptor, and can be an agent for preventing and/or treating diseases related to a cannabinoid type 2 receptor such as inflammatory diseases, pain, and the like.
摘要翻译：基于对大麻素2型受体的激动作用，预防和/或治疗与大麻素2型受体相关的疾病的新颖且优异的方法。发现主要具有两个取代基的杂环衍生物，例如2-位具有取代基氨基的嘧啶-5-甲酰胺衍生物对大麻素2型受体表现出强烈的激动作用，并且可以是用于预防和/或治疗与大麻素2型受体相关的疾病如炎性疾病，疼痛等的药剂。

7. 发明申请

US20110053912A1 PYRIMIDINE COMPOUND 有权
标题翻译：吡嗪化合物
公开(公告)号：US20110053912A1
公开(公告)日：2011-03-03
申请号：US12933137
申请日：2010-03-29
申请人： Yuji Matsushima , Hirokazu Kubota , Hisao Hamaguchi , Yoshinori Okamoto , Takeshi Hondo , Fusako Nishigaki
发明人： Yuji Matsushima , Hirokazu Kubota , Hisao Hamaguchi , Yoshinori Okamoto , Takeshi Hondo , Fusako Nishigaki
IPC分类号： A61K31/55 , C07D405/12 , A61K31/506 , A61P29/00 , C07D413/12 , A61K31/5377 , C07D417/12 , A61K31/541 , C07D491/107 , C07D417/14
CPC分类号： C07D239/42 , C07D239/34 , C07D239/38 , C07D239/48 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/06 , C07D451/04 , C07D453/02 , C07D491/107 , C07D493/08
摘要： A novel and excellent method for preventing and/or treating diseases related to a cannabinoid type 2 receptor, based on an agonistic action on a cannabinoid type 2 receptor. It was found that a hetero ring derivative mainly having two substituents, for example, a pyrimidine-5-carboxamide derivative having a substituent amino group at the 2-position, exhibits a potent agonistic action on a cannabinoid type 2 receptor, and can be an agent for preventing and/or treating diseases related to a cannabinoid type 2 receptor such as inflammatory diseases, pain, and the like.
摘要翻译：基于对大麻素2型受体的激动作用，预防和/或治疗与大麻素2型受体相关的疾病的新颖且优异的方法。发现主要具有两个取代基的杂环衍生物，例如2-位具有取代基氨基的嘧啶-5-甲酰胺衍生物对大麻素2型受体表现出强烈的激动作用，并且可以是用于预防和/或治疗与大麻素2型受体相关的疾病如炎性疾病，疼痛等的药剂。

8. 发明授权

US07407961B2 Pyrazine derivatives and pharmaceutical use thereof 失效
标题翻译：吡嗪衍生物及其药物用途
公开(公告)号：US07407961B2
公开(公告)日：2008-08-05
申请号：US10972340
申请日：2004-10-26
申请人： Satoshi Yonishi , Satoshi Aoki , Yuji Matsushima , Atsushi Akahane
发明人： Satoshi Yonishi , Satoshi Aoki , Yuji Matsushima , Atsushi Akahane
IPC分类号： A61K31/4965 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14
摘要： A pyrazine derivative of the following formula (I): or a salt thereof. The pyrazine compound (I) and a salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.
摘要翻译：下式（I）的吡嗪衍生物或其盐。本发明的吡嗪化合物（I）及其盐是腺苷拮抗剂，可用于预防和/或治疗抑郁症，痴呆（例如阿尔茨海默氏病，脑血管性痴呆，伴有帕金森病的痴呆等），帕金森病，焦虑，疼痛，脑血管疾病（例如中风等），心力衰竭等。

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